中文同义词:
维多珠单抗;VEDOLIZUMAB ( 维多组单抗 );维多组单抗
英文同义词:
Vedolizumab;Vedolizumab USP/EP/BP
生物活性
Vedolizumab是一种靶向α4β7整联蛋白 (integrin) 的人源化单克隆抗体，用于溃疡性结肠炎和克罗恩病的相关研究。
体外研究
Vedolizumab does not bind to the majority of memory CD4+ T lymphocytes (60%), neutrophils, and most monocytes. The highest level of vedolizumab binding is to a subset (25%) of human peripheral blood memory CD4+ T lymphocytes that include gut-homing interleukin 17 T-helper lymphocytes. Vedolizumab also binds to eosinophils at high levels, and to naive T-helper lymphocytes, naive and memory cytotoxic T lymphocytes, B lymphocytes, natural killer cells, and basophils at lower levels; vedolizumab binds to memory CD4+ T and B lymphocytes with subnanomolar potency (EC 50 =0.3-0.4 nM). Vedolizumab selectively inhibits adhesion of α4β7-expressing cells to mucosal addressin cell adhesion molecule 1 (IC 50 =0.02-0.06 g/mL) and fibronectin (IC 50 =0.02 g/mL), but not vascular cell adhesion molecule 1.
体内研究
Blockade of α4β7 receptors on T-lymphocytes has been shown to occur for several weeks after a single dose of vedolizumab. The drug concentration following the infusion has been shown to be dose related with a mean maximum concentration of 12.5 μg/mL in those receiving 0.5 mg/kg of vedolizumab and 52.0 μg/mL in those receiving 2 mg/kg. The serum half-life of these two doses is 9-12 days respectively and saturation of α4β7 receptors on T-lymphocytes is >90% at both 4-6 weeks following infusion. In a dose ranging study, the serum drug concentrations increase with increasing dose and when regular induction infusions are used (on day 1, 15, 29 and 85), the serum half-life is between 15 and 22 days across all groups.
